Substances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.

RELATED TERMS--------------------------------------

ReceptorA molecule that recognizes a unique hormone. Once that hormone is bound to the receptor, the information carried by the hormone can now exert its biological action.

SIMILAR TERMS--------------------------------------

GABAAn amino acid that is found in the central nervous system; acts as an inhibitory neurotransmitter.

GABA A ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA A ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA AgentsSubstances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.

GABA alpha Ketoglutarate AminotransferaseAn enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.

GABA AminotransferaseAn enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.

GABA AntagonistDrugs that bind to but do not activate GAMMA-AMINOBUTYRIC ACID receptors, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID or GAMMA-AMINOBUTYRIC ACID agonists.

GABA AntagonistsDrugs that bind to but do not activate GAMMA-AMINOBUTYRIC ACID receptors, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID or GAMMA-AMINOBUTYRIC ACID agonists.

GABA B ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and influence cells via interactions with G-proteins. GABA-B receptors are pharmacologically characterized by their insensitivity to the blocker bicuculline and sensitivity to the agonist L-baclofen. They are found both presynaptically and postsynaptically, and act variously by inhibition of adenylate cyclase, activation of phospholipase A2, activation of potassium channels, and inactivation of voltage-activated calcium channels.

GABA B ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and influence cells via interactions with G-proteins. GABA-B receptors are pharmacologically characterized by their insensitivity to the blocker bicuculline and sensitivity to the agonist L-baclofen. They are found both presynaptically and postsynaptically, and act variously by inhibition of adenylate cyclase, activation of phospholipase A2, activation of potassium channels, and inactivation of voltage-activated calcium channels.

GABA Benzodiazepine ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA Benzodiazepine ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA ModulatorsSubstances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act. General anesthetics probably act at least partly by potentiating GABAergic responses, but they are not included here.

GABA ReceptorCell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.

GABA Receptor AntagonistsDrugs that bind to but do not activate GAMMA-AMINOBUTYRIC ACID receptors, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID or GAMMA-AMINOBUTYRIC ACID agonists.

GABA ReceptorsCell-surface proteins that bind GAMMA-AMINOBUTYRIC ACID with high affinity and trigger changes that influence the behavior of cells. GABA-A receptors control chloride channels formed by the receptor complex itself. They are blocked by bicuculline and usually have modulatory sites sensitive to benzodiazepines and barbiturates. GABA-B receptors act through G-proteins on several effector systems, are insensitive to bicuculline, and have a high affinity for L-baclofen.

GABA TransaminaseAn enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.

GABA(A) ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA, ChlorophenylA GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist at GABA-B receptors (RECEPTORS, GABA-B). It is used in the treatment of spasticity, especially that due to spinal cord damage. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

GABA, LithiumThe most common inhibitory neurotransmitter in the central nervous system.

GABA-A ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA-A ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA-alpha-Ketoglutarate AminotransferaseAn enzyme that converts brain gamma-aminobutyric acid (GAMMA-AMINOBUTYRIC ACID) into succinate semialdehyde, which can be converted to succinic acid and enter the citric acid cycle. It also acts on beta-alanine. EC 2.6.1.19.

GABA-B ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and influence cells via interactions with G-proteins. GABA-B receptors are pharmacologically characterized by their insensitivity to the blocker bicuculline and sensitivity to the agonist L-baclofen. They are found both presynaptically and postsynaptically, and act variously by inhibition of adenylate cyclase, activation of phospholipase A2, activation of potassium channels, and inactivation of voltage-activated calcium channels.

GABA-B ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and influence cells via interactions with G-proteins. GABA-B receptors are pharmacologically characterized by their insensitivity to the blocker bicuculline and sensitivity to the agonist L-baclofen. They are found both presynaptically and postsynaptically, and act variously by inhibition of adenylate cyclase, activation of phospholipase A2, activation of potassium channels, and inactivation of voltage-activated calcium channels.

GABA-Benzodiazepine ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA-Benzodiazepine ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABAergic AgentSubstances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.

GABAergic ModulatorsSubstances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act. General anesthetics probably act at least partly by potentiating GABAergic responses, but they are not included here.

GabapentinGabapentin is a prescription or over-the-counter drug which is (or once was) approved in the United States and possibly in other countries. Active ingredient(s): gabapentin.

GabapetinGabapetin is a prescription or over-the-counter drug which is (or once was) approved in the United States and possibly in other countries. Active ingredient(s): gabapentin.

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Gabexate MonomethanesulfonateA serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

Gabexate MesylateA serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

Gabexate MesilateA serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

GabexateA serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

GabbromycinAn oligosaccharide antibiotic produced by various Streptomyces.

GABAergic Agents

GABAergic ModulatorsSubstances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act. General anesthetics probably act at least partly by potentiating GABAergic responses, but they are not included here.

GABAergic AgentSubstances used for their pharmacological actions on GABAergic systems. GABAergic agents include agonists, antagonists, degradation or uptake inhibitors, depleters, precursors, and modulators of receptor function.

GABA-Benzodiazepine ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA-Benzodiazepine ReceptorCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and control an integral membrane chloride channel. GABA-A receptors are the most prevalent inhibitory neurotransmitter receptors in the brain. Several isoforms have been cloned, and they belong to a superfamily which includes nicotinic receptors, glycine receptors, and 5HT-3 receptors. Most GABA-A receptors have separate modulatory sites sensitive to benzodiazepines and to barbiturates.

GABA-B ReceptorsCell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and influence cells via interactions with G-proteins. GABA-B receptors are pharmacologically characterized by their insensitivity to the blocker bicuculline and sensitivity to the agonist L-baclofen. They are found both presynaptically and postsynaptically, and act variously by inhibition of adenylate cyclase, activation of phospholipase A2, activation of potassium channels, and inactivation of voltage-activated calcium channels.

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